Drug intelligence / Profile preview

calcitriol + gemcitabine + erlotinib

Development stage
Unknown
Lead developer
Roche
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Calcitriol + gemcitabine + erlotinib is a combination regimen investigated primarily for the treatment of advanced pancreatic cancer. Calcitriol is the hormonally active form of vitamin D3 and acts as a vitamin D receptor agonist with potential anti-proliferative effects. Gemcitabine is a nucleoside analog that inhibits DNA synthesis by incorporating into DNA and inhibiting ribonucleotide reductase, leading to cell death in rapidly dividing cells. Erlotinib is an orally active small molecule inhibitor of the epidermal growth factor receptor tyrosine kinase (EGFR), blocking downstream signaling pathways involved in tumor cell proliferation and survival[2][5][7]. The combination has been studied in clinical trials to assess whether adding high-dose calcitriol to standard chemotherapy with gemcitabine ± erlotinib improves outcomes for patients with advanced pancreatic cancer[2]. While each agent has distinct mechanisms—calcitriol modulates gene expression via the vitamin D receptor; gemcitabine disrupts DNA replication; and erlotinib inhibits EGFR signaling—their combined use aims to enhance anti-tumor efficacy through complementary actions.

Other names
DN-101 (for high-dose calcitriol)CP 358774 (erlotinib)OSI 774 (erlotinib)NSC 718781 (erlotinib)R 1415 (erlotinib)
02

Targets

DNA polymerase familyEGFR (Epidermal growth factor receptor)VDR (Vitamin D receptor)RNR (Ribonucleotide reductase)

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